ASTX029

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ASTX029

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Cat No: 33557

Biochemicals - Kinase Inhibitors

ASTX029 is an ERK inhibitor (IC50 = 2.7 nM for ERK2).{62100} It is selective for ERK over a panel of 465 kinases. ASTX029 reduces phosphorylation of p90 ribosomal S6 kinase (RSK) in mutant B-RAF-expressing A375 melanoma and mutant K-Ras-expressing HCT...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

(?R)-6-[5-chloro-2-[(tetrahydro-2H-pyran-4-yl)amino]-4-pyrimidinyl]-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]-1,3-dihydro-?-methyl-1-oxo-2H-isoindole-2-acetamide

Correlated keywords:

ASTX-029 Calu6 COLO205 HCT-116

Product Overview:
ASTX029 is an ERK inhibitor (IC50 = 2.7 nM for ERK2).{62100} It is selective for ERK over a panel of 465 kinases. ASTX029 reduces phosphorylation of p90 ribosomal S6 kinase (RSK) in mutant B-RAF-expressing A375 melanoma and mutant K-Ras-expressing HCT116 colorectal cancer cells with IC50 values of 3.3 and 4 nM, respectively. It inhibits proliferation in a panel of cancer cell lines, including melanoma, colorectal, and lung cancer cells. ASTX029 reduces tumor growth in A375, Calu-6, and COLO 205 mouse xenograft models.

Size	500 µg
Shipping	dry ice
CAS Number	2095719-92-7
Molecular Formula	C₂₉H₃₁ClFN₅O₅
SMILES	O=C1C2=CC(C3=NC(NC4CCOCC4)=NC=C3Cl)=CC=C2CN1[C@H](C)C(N[C@@H](C5=CC(OC)=CC(F)=C5)CO)=O
Molecular Weight	584
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.79
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.